It is becoming increasingly recognized that increased inflammation is strongly associated with, if not the underlying cause of, many disease conditions including obesity, type 2 diabetes, cancer, heart disease, and neurological conditions such as multiple sclerosis and Alzheimer's disease.
It has been shown that the regulation of certain eicosanoids, a class of biologically active metabolites, can help control inflammation. While many anti-inflammatory drugs directly target the production of pro-inflammatory eicosanoids, e.g., by inhibiting the enzyme required in their production, an alternative and more sophisticated approach would be to reduce the amount of substrate upstream in the pathway, i.e., by regulating the formation of the precursors of pro-inflammatory cicosanoids, namely arachidonic acid (AA). Since AA is produced by the enzyme Δ-5-desaturase (D5D), the synthesis and/or identification of specific inhibitors of D5D can help to treat, moderate, and prevent inflammation. U.S. Pat. No. 6,172,106, the entire disclosure of which is incorporated by reference herein, has identified sesamol as a specific inhibitor of D5D. Unfortunately, sesamol is believed to be potentially toxic. Additionally, although natural compounds such as sesame lignans and curcumin have been demonstrated to exhibit inhibitory activity on D5D, their complex structures make them difficult to synthesize. Furthermore, sesame lignans also have potential toxicity. Hence, there is a need to develop non-toxic inhibitors of D5D that are easy to synthesize and can he produced on an industrial scale.